mGluR Agonist

L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively.

L-Glutamine-¹⁵N₂,d₅ is the deuterium and ¹⁵N-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC₅₀s in the 2 to 5 μM range.

VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a K_i of 156 nM and an EC₅₀ of 9.6 nM.

(2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC hydrate affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC hydrate can be used in the study of epilepsy and other neurological diseases.

LY2812223 is a highly potent, functionally selective mGlu₂ receptor agonist with mGlu₂ binding affinity for mGlu₂ and mGlu₃ (K_i=144 nM and 156 nM, respectively).

L-Glutamine-d₄ (L-Glutamic acid 5-amide-d₄) is the deuterium labeled L-Glutamine (HY-N0390). L-Glutamine is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells.

Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders.

VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC₅₀s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with K_i values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.

VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC₅₀ value of 16 nM and a K_i of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice.

Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.

(2R,4R)-APDC is a group II metabotropic glutamate receptor (mGluR) agonist. (2R,4R)-APDC affects cell proliferation by inhibiting glutamate release, enhancing motor responses produced by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. (2R,4R)-APDC can be used in the study of epilepsy and other neurological diseases.

LY2979165 is the alanine proagent of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.

CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC₅₀: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease, such as Parkinson's disease (PD).

L-Cysteinesulfinic acid (Standard) is the analytical standard of L-Cysteinesulfinic acid. This product is intended for research and analytical applications. L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC₅₀ of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.

Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia.

MGS0274, an ester-based lipophilic proagent of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia.

Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC₅₀ of 79 nM. Antiparkinsonian effect.

DL-AP4 sodium (2-Amino-4-phosphonobutyric acid sodium) is an agonist for metabotropic glutamate receptors (mGluR). DL-AP4 sodium binds to mGluR4, activates the signaling pathway that is negatively correlated with adenylate cyclase, and inhibits the Forskolin (HY-15371)-induced production of cAMP. DL-AP4 sodium is also an inhibitor for ON channel, that reduces the sensitivity of photoreceptors to brightness changes.